5-(2'-hydroxyphenyl)isothiazole | 120869-47-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 英文名称: 5-(2'-hydroxyphenyl)isothiazole
• 英文别名: 2-(5-Isothiazolyl)phenol；2-(1,2-thiazol-5-yl)phenol
• CAS: 120869-47-8
• 化学式: C₉H₇NOS
• 分子量: 177.227
• InChiKey: UYSSACLVCFURJI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  61.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-(2'-hydroxyphenyl)isothiazole 在 sodium hydride 作用下， 以 四氢呋喃 为溶剂， 生成 5-[2-(4,5-dihydro-1H-imidazol-2-ylmethoxy)phenyl]-1,2-thiazole
  参考文献：
  名称：

  α1-Adrenoceptor Agonists: The Identification of Novel α1A Subtype Selective 2′-Heteroaryl-2-(phenoxymethyl)imidazolines

  摘要：

  Novel 2'-heteroaryl-2-(phenoxymethyl)imidazolines have been identified as potent agonists of the cloned human alpha(1)-adrenoceptors in vitro. The nature of the 2'-heteroaryl group can have significant effects on the potency, efficacy, and subtype selectivity in this series. alpha(1A) Subtype selective agonists have been identified. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(01)00764-8
• 作为产物：
  描述：

  色酮 在 劳森试剂 、 S,S-二苯基硫亚胺 作用下， 以 氯仿 、 甲苯 为溶剂， 生成 5-(2'-hydroxyphenyl)isothiazole
  参考文献：
  名称：

  α1-Adrenoceptor Agonists: The Identification of Novel α1A Subtype Selective 2′-Heteroaryl-2-(phenoxymethyl)imidazolines

  摘要：

  Novel 2'-heteroaryl-2-(phenoxymethyl)imidazolines have been identified as potent agonists of the cloned human alpha(1)-adrenoceptors in vitro. The nature of the 2'-heteroaryl group can have significant effects on the potency, efficacy, and subtype selectivity in this series. alpha(1A) Subtype selective agonists have been identified. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(01)00764-8

文献信息

• Beta 3 adrenergic agonists
  申请人：Sall Jon Daniel

  公开号：US20050080110A1

  公开（公告）日：2005-04-14

  The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g., for treating Type 2 diabetes and/or obesity.

  本发明涉及一种β3肾上腺素能受体激动剂，其化学式为（I）；或其药用盐；该激动剂能够增加细胞中的脂解和能量消耗，因此，它可以用于治疗2型糖尿病和/或肥胖等疾病。
• Beta3 adrenergic agonists
  申请人：——

  公开号：US20030191156A1

  公开（公告）日：2003-10-09

  The present invention relates to a &bgr; 3 adrenergic receptor agonist of formula (I) or a pharmaceutical salt thereof, which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type II diabetes and/or obesity. The compound can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compound can be used to reduced neurogenic inflammation or as an antidepressant agent. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.

  本发明涉及一种式(I)的&bgr;3肾上腺素受体激动剂或其药物盐，该激动剂能够增加细胞的脂解和能量消耗，因此可用于治疗II型糖尿病和/或肥胖症。该化合物还可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道蠕动。此外，该化合物还可用于减少神经源性炎症或作为抗抑郁剂。还公开了在治疗糖尿病和肥胖症以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道蠕动方面使用该化合物的组合物和方法。
• Buggle, Katherine; Fallon, Bernadette, Journal of Chemical Research, Miniprint, 1988, # 11, p. 2764 - 2784
  作者：Buggle, Katherine、Fallon, Bernadette

  DOI：——

  日期：——
• BUGGLE, KATHERINE;FALLON, BERNADETTE
  作者：BUGGLE, KATHERINE、FALLON, BERNADETTE

  DOI：——

  日期：——
• INDOLE DERIVATIVES AS BETA-3 ADRENERGIC AGONISTS FOR THE TREATMENT OF TYPE 2 DIABETES
  申请人：ELI LILLY AND COMPANY

  公开号：EP1421078B1

  公开（公告）日：2006-09-27